WO2019023651A3 - Modulateurs du récepteur des androgènes à petite molécule - Google Patents
Modulateurs du récepteur des androgènes à petite molécule Download PDFInfo
- Publication number
- WO2019023651A3 WO2019023651A3 PCT/US2018/044204 US2018044204W WO2019023651A3 WO 2019023651 A3 WO2019023651 A3 WO 2019023651A3 US 2018044204 W US2018044204 W US 2018044204W WO 2019023651 A3 WO2019023651 A3 WO 2019023651A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- androgen receptor
- small molecule
- molecule modulators
- compounds
- useful
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/40—Oxygen atoms
- C07D211/44—Oxygen atoms attached in position 4
- C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Abstract
La présente invention concerne des composés utiles pour moduler l'activité d'un récepteur d'androgène, ou un variant de celui-ci, et des compositions et des procédés associés. Les composés de l'invention sont utiles pour exercer un effet antagoniste du variant d'épissage de récepteur d'androgène AR-v7, et pour le traitement du cancer de la prostate résistant à la castration.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US16/198,553 US10961216B2 (en) | 2017-07-28 | 2018-11-21 | Small molecule modulators of the androgen receptor |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201762538471P | 2017-07-28 | 2017-07-28 | |
US62/538,471 | 2017-07-28 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
US16/198,553 Continuation US10961216B2 (en) | 2017-07-28 | 2018-11-21 | Small molecule modulators of the androgen receptor |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2019023651A2 WO2019023651A2 (fr) | 2019-01-31 |
WO2019023651A3 true WO2019023651A3 (fr) | 2019-03-28 |
Family
ID=63209673
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/US2018/044204 WO2019023651A2 (fr) | 2017-07-28 | 2018-07-27 | Modulateurs du récepteur des androgènes à petite molécule |
Country Status (2)
Country | Link |
---|---|
US (1) | US10961216B2 (fr) |
WO (1) | WO2019023651A2 (fr) |
Families Citing this family (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2016141458A1 (fr) | 2015-03-12 | 2016-09-15 | British Columbia Cancer Agency Branch | Dérivés d'éther de bisphénol et leurs procédés d'utilisation |
US10865184B2 (en) | 2015-04-21 | 2020-12-15 | University Of Tennessee Research Foundation | Selective androgen receptor degrader (SARD) ligands and methods of use thereof |
US20170298033A1 (en) | 2016-04-15 | 2017-10-19 | The University Of British Columbia | Bisphenol derivatives and their use as androgen receptor activity modulators |
GB201914296D0 (en) * | 2019-10-03 | 2019-11-20 | Univ Oxford Innovation Ltd | Treatment |
CN115427028A (zh) * | 2020-02-25 | 2022-12-02 | 田纳西大学研究基金会 | 选择性雄激素受体共价拮抗剂(sarca)及其使用方法 |
CN115916170A (zh) | 2020-04-17 | 2023-04-04 | 埃萨制药股份有限公司 | 固体形式的n-末端结构域雄激素受体抑制剂及其用途 |
US20220380378A1 (en) * | 2021-04-22 | 2022-12-01 | Essa Pharma, Inc. | Androgen receptor modulators and methods for their use |
IL309666A (en) | 2021-07-09 | 2024-02-01 | Plexium Inc | Aryl compounds and pharmaceutical preparations that modulate IKZF2 |
Citations (12)
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EP1329454A1 (fr) * | 2000-09-29 | 2003-07-23 | Nippon Soda Co., Ltd. | Composes de thienopyrimidine et leurs sels et procede de preparation |
WO2005042537A1 (fr) * | 2003-10-22 | 2005-05-12 | Bristol-Myers Squibb Company | Composes bicycliques a substitution phenyl-aniline utilises comme inhibiteur de la kinase |
US20060167053A1 (en) * | 2003-02-26 | 2006-07-27 | Tomoharu Iino | Heteroarylcarbamoylbenzene derivative |
WO2006124874A2 (fr) * | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibiteurs de la b-raf kinase |
US20080108611A1 (en) * | 2006-01-19 | 2008-05-08 | Battista Kathleen A | Substituted thienopyrimidine kinase inhibitors |
WO2011104337A1 (fr) * | 2010-02-26 | 2011-09-01 | Boehringer Ingelheim International Gmbh | Thiénopyrimidines contenant un groupe hétérocycloalkyle pour des compositions pharmaceutiques |
US8053447B2 (en) * | 2006-04-07 | 2011-11-08 | High Point Pharmaceuticals, Llc | 11β-hydroxysteroid dehydrogenase type 1 active compounds |
WO2013116491A1 (fr) * | 2012-02-01 | 2013-08-08 | Rigel Pharmaceuticals, Inc. | Composés de carboxamide, de sulfonamide et d'amine et procédés pour utiliser ceux-ci |
WO2017041040A1 (fr) * | 2015-09-04 | 2017-03-09 | City Of Hope | Antagonistes du récepteur des androgènes |
US20170095446A1 (en) * | 2015-04-21 | 2017-04-06 | Gtx, Inc. | Selective androgen receptor degrader (sard) ligands and methods of use thereof |
US20170152260A1 (en) * | 2013-01-15 | 2017-06-01 | Board Of Regents, The University Of Texas System | Stat3 inhibitor |
WO2017165908A1 (fr) * | 2016-03-31 | 2017-10-05 | South Australian Health And Medical Research Institute Limited | Procédé d'inhibition d'états associés à un régime riche en matières grasses |
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CN101384757A (zh) | 2006-01-03 | 2009-03-11 | 哈佛大学校长及研究员协会 | 小分子印渍 |
WO2011044327A1 (fr) | 2009-10-07 | 2011-04-14 | Medivation Prostate Therapeutics, Inc. | Composés de phénylcarbamoyl alkylamino arènes substitués et composés de n,n'-bis-arylurée |
ES2555393T3 (es) * | 2009-12-18 | 2015-12-30 | Glaxosmithkline Intellectual Property Limited | Nuevos compuestos |
CA2791114A1 (fr) * | 2010-02-26 | 2011-09-01 | Boehringer Ingelheim International Gmbh | Thienopyrimidines contenant un groupe alkyle substitue pour des compositions pharmaceutiques |
CN102858782A (zh) * | 2010-02-26 | 2013-01-02 | 贝林格尔.英格海姆国际有限公司 | 用于药物组合物的具有Mnk1/Mnk2 抑制活性的4-[环烷基氧基(杂)芳基氨基]噻吩并[2,3-d]嘧啶 |
SG11201507093WA (en) | 2013-03-14 | 2015-10-29 | Univ Maryland Baltimore Office Of Technology Transfer | Androgen receptor down-regulating agents and uses thereof |
CN105636594A (zh) | 2013-08-12 | 2016-06-01 | 托凯药业股份有限公司 | 使用雄激素靶向疗法用于***性疾病的生物标记物 |
CA2844640A1 (fr) | 2013-12-06 | 2015-06-06 | The University Of British Columbia | Procede de traitement du cancer de la prostate resistant a la castration |
CA2939048A1 (fr) | 2014-02-14 | 2015-08-20 | The University Of British Columbia | Composes ciblant le domaine de liaison a l'adn (dbd) du recepteur des androgenes humain servant d'agents therapeutiques et procedes pour leur utilisation |
WO2015150921A2 (fr) | 2014-04-03 | 2015-10-08 | Fundacio Institut De Recerca Biomedica (Irb Barcelona) | Procédés de traitement du cancer de la prostate |
KR20160138136A (ko) * | 2014-04-15 | 2016-12-02 | 연세대학교 산학협력단 | 티에노피리미딘 유도체 또는 이의 약학적으로 허용가능한 염을 포함하는 백혈병 치료 및 예방용 약학 조성물 |
WO2016049774A1 (fr) | 2014-10-03 | 2016-04-07 | The Royal Institution For The Advancement Of Learning/Mcgill University | Urée et composés à base de bis-urée et analogues de ceux-ci utiles dans le traitement de maladies ou trouble à médiation par récepteur des androgènes |
GB201421933D0 (en) | 2014-12-10 | 2015-01-21 | Singapore Volition Pte Ltd | Method for a detection of hormone sensitive diease progression |
EP3268087A4 (fr) | 2015-03-12 | 2018-08-29 | The Regents of the University of California | Méthodes de traitement du cancer par des inhibiteurs de ror gamma |
US10173978B2 (en) | 2015-08-05 | 2019-01-08 | Georgetown University | Small molecule androgen receptor inhibitors and methods of use thereof |
WO2017066697A1 (fr) | 2015-10-14 | 2017-04-20 | Dou Qingping | Traitements et diagnostics de cancers |
US20190060296A1 (en) | 2017-07-28 | 2019-02-28 | Massachusetts Institute Of Technology | Discovery of small molecules that target the androgen receptor and uses |
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2018
- 2018-07-27 WO PCT/US2018/044204 patent/WO2019023651A2/fr active Application Filing
- 2018-11-21 US US16/198,553 patent/US10961216B2/en active Active
Patent Citations (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1329454A1 (fr) * | 2000-09-29 | 2003-07-23 | Nippon Soda Co., Ltd. | Composes de thienopyrimidine et leurs sels et procede de preparation |
US20060167053A1 (en) * | 2003-02-26 | 2006-07-27 | Tomoharu Iino | Heteroarylcarbamoylbenzene derivative |
WO2005042537A1 (fr) * | 2003-10-22 | 2005-05-12 | Bristol-Myers Squibb Company | Composes bicycliques a substitution phenyl-aniline utilises comme inhibiteur de la kinase |
WO2006124874A2 (fr) * | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibiteurs de la b-raf kinase |
US20080108611A1 (en) * | 2006-01-19 | 2008-05-08 | Battista Kathleen A | Substituted thienopyrimidine kinase inhibitors |
US8053447B2 (en) * | 2006-04-07 | 2011-11-08 | High Point Pharmaceuticals, Llc | 11β-hydroxysteroid dehydrogenase type 1 active compounds |
WO2011104337A1 (fr) * | 2010-02-26 | 2011-09-01 | Boehringer Ingelheim International Gmbh | Thiénopyrimidines contenant un groupe hétérocycloalkyle pour des compositions pharmaceutiques |
WO2013116491A1 (fr) * | 2012-02-01 | 2013-08-08 | Rigel Pharmaceuticals, Inc. | Composés de carboxamide, de sulfonamide et d'amine et procédés pour utiliser ceux-ci |
US20170152260A1 (en) * | 2013-01-15 | 2017-06-01 | Board Of Regents, The University Of Texas System | Stat3 inhibitor |
US20170095446A1 (en) * | 2015-04-21 | 2017-04-06 | Gtx, Inc. | Selective androgen receptor degrader (sard) ligands and methods of use thereof |
WO2017041040A1 (fr) * | 2015-09-04 | 2017-03-09 | City Of Hope | Antagonistes du récepteur des androgènes |
WO2017165908A1 (fr) * | 2016-03-31 | 2017-10-05 | South Australian Health And Medical Research Institute Limited | Procédé d'inhibition d'états associés à un régime riche en matières grasses |
Non-Patent Citations (2)
Title |
---|
KUSH DALAL ET AL: "Selectively Targeting the DNA-binding Domain of the Androgen Receptor as a Prospective Therapy for Prostate Cancer", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 289, no. 38, 19 September 2014 (2014-09-19), US, pages 26417 - 26429, XP055357599, ISSN: 0021-9258, DOI: 10.1074/jbc.M114.553818 * |
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Also Published As
Publication number | Publication date |
---|---|
WO2019023651A2 (fr) | 2019-01-31 |
US10961216B2 (en) | 2021-03-30 |
US20190202800A1 (en) | 2019-07-04 |
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